Topical compositions and methods for skin lightening

a composition and skin technology, applied in the field of dermatological compositions and methods, can solve the problems that the use of histamine antagonists to reduce pigmentation has received little attention to date, and achieve the effects of reducing pigmentation in human skin, reducing histamine-induced pigmentation, and reducing the appearance of liver spots, freckles, and mottled and discrete pigmentation

Inactive Publication Date: 2016-09-15
AVON PROD INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0005]In accordance with the foregoing objectives and others, the invention provides compounds, topical compositions and methods for reducing pigmentation in human skin. Without wishing to be bound by any theory, it is believed that the compounds of the invention are histamine receptor (e.g., H1, H2, H3 and / or H4 receptor) antagonists effective to reduce histamine-induced pigmentation in human skin. In some implementations, new H2 receptor antagonists are provided. The compositions and methods may treat hyperpigmentation conditions, including those associated with UV damage, inflammation, and chronological aging, including without limitation treating, ameliorating, diminishing the appearance of, or preventing age spots, liver spots, freckles, mottled and discrete pigmentation, melasma and the like. The compositions and methods are also useful for reducing otherwise unwanted pigmentation, including overall lightening of the skin, as well as improving signs of chronological, environmental, or UV skin aging.

Problems solved by technology

However, the use of histamine antagonists to reduce pigmentation has received little attention to date.

Method used

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  • Topical compositions and methods for skin lightening
  • Topical compositions and methods for skin lightening
  • Topical compositions and methods for skin lightening

Examples

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Effect test

example 1

[0100]The Compound of Formula (II) was examined for its ability to reduce pigmentation in vitro in human melanocytes. Human epidermal melanocytes from dark-pigmented skin were seeded in 6-well dishes and grown using commercially available Medium 254, a sterile, liquid medium prepared with 200 μM calcium chloride for the culture of human epidermal melanocytes, supplemented with 1% Penicillin / Streptomycin and 1% Human Melanocyte Growth Supplement. Histamine, Diphenhydramine HCl and Compound II were added to the growth medium at the concentrations listed in Table 1 below. Corresponding controls were maintained without histamine, Diphenylhydramine HCl and Compound II. Four replicates were tested for each combination. After 8 days of incubation, melanin was collected and processed by washing the wells with IX phosphate-buffered saline (PBS), followed by addition of 200 μL of 2M NaOH to three of the four replicates, which are then scraped, pooled and boiled at 80° C. for an hour. Melanin ...

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Abstract

Embodiments of the invention are generally directed to compositions useful for reducing pigmentation in the skin. The composition may further include other depigmenting agents such as nicotinamide and its melanasome transfer-inhibiting derivatives, 3,3′-thiodipropanoic acid and its tyrosinase-inhibiting derivatives, or resorcinol and its tyrosinase-inhibiting derivatives, in a topically acceptable vehicle.

Description

FIELD OF INVENTION[0001]The invention relates generally to cosmetic and dermatological compositions and methods for reducing pigmentation in human integuments. More particularly, the invention provides topical compositions and associated methods for treatment of hyperpigmentation or reduction of unwanted pigmentation. The compositions may be applied topically to skin to reduce pigmentation in the area of application.BACKGROUND[0002]The color of human skin is due primarily to the production of melanin by specialized cells in the skin called melanocytes through a process known as melanogenesis. The synthesis of melanin is a complex process involving several biochemical pathways. It is generally recognized that pigmentation may accompany inflammatory processes. Histamine is an agent involved in the inflammatory response which is reported to increase tyrosinase activity in human melanocytes, with the effects being completely inhibited by histamine antagonists such as famotidine. Histami...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K8/49A61Q19/02A61K8/46A61K8/36A61K8/06A61K8/34
CPCA61K8/4926A61K8/06A61K8/064A61K8/062A61K8/342A61K8/46A61K2800/524A61K8/36A61Q19/02A61K2800/48A61K2800/54A61K2800/42A61K2800/522A61K8/347A61K8/675A61P17/00A61K8/49
Inventor HU, HONGYIM, SUNGHANSANTHANAM, UMALYGA, JOHN W.
Owner AVON PROD INC
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